title: Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.
abstract: Novel multi-target-directed ligands were designed by replacing the inner dipiperidino function of 3 with less flexible or completely rigid moieties to obtain compounds endowed with multiple biological properties that might be relevant to Alzheimer's disease. 15 was the most interesting, inhibiting AChE in the nanomolar range and inhibiting AChE-induced and self-promoted beta-amyloid aggregation in the micromolar range.
authors.affiliation: Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy. vincenzo.tumiatti@unibo.it
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Tumiatti
authors.forename: Andrea
authors.initials: A
authors.lastname: Milelli
authors.forename: Anna
authors.initials: A
authors.lastname: Minarini
authors.forename: Michela
authors.initials: M
authors.lastname: Rosini
authors.forename: Maria Laura
authors.initials: ML
authors.lastname: Bolognesi
authors.forename: Marialuisa
authors.initials: M
authors.lastname: Micco
authors.forename: Vincenza
authors.initials: V
authors.lastname: Andrisano
authors.forename: Manuela
authors.initials: M
authors.lastname: Bartolini
authors.forename: Francesca
authors.initials: F
authors.lastname: Mancini
authors.forename: Maurizio
authors.initials: M
authors.lastname: Recanatini
authors.forename: Andrea
authors.initials: A
authors.lastname: Cavalli
authors.forename: Carlo
authors.initials: C
authors.lastname: Melchiorre
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism*; D016229:Amyloid beta-Peptides / Q000737:chemistry / Q000378:metabolism; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D008024:Ligands; D015394:Molecular Structure; D011073:Polyamines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D016229:Amyloid beta-Peptides; D002800:Cholinesterase Inhibitors; D008024:Ligands; D011073:Polyamines; D000110:Acetylcholinesterase